EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC₅₀ of 3.9 nM.

IC50: 3.9 nM (MEK)^[1]

504.22

C₁₈H₁₅F₂IN₂O₅

1801896-05-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Lu B, et al. Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold. Bioorg Med Chem. 2018 Feb 1;26(3):581-589.

EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC₅₀ of 6 nM in Pfeffiera cell lines, respectively.

IC50: 6 nM (EZH2)^[1].

EBI-2511 (Compound 34) significantly reduces cellular H3K27me3 levels in a dose-dependent manner with an approximate IC₅₀ of 8 nM, which is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active with IC₅₀ value of 55 nM against WSU-DLCL2^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

EBI-2511 displays a dose-dependent inhibition on the tumor growth, resulting in 28% (10mg/kg), 83% (30mg/kg), and 97% (100mg/kg) reduction in tumor size. At the same dosage level, EBI-2511 shows a superior anti-tumor efficacy to EPZ-6438 (P<0.01). It is noteworthy that no significant changes in body weights of all treatment groups are observed^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

576.77

C₃₄H₄₈N₄O₄

2098546-05-3

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 5 mg/mL (8.67 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 0.5 mg/mL (0.87 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (0.87 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 0.5 mg/mL (0.87 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (0.87 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 0.5 mg/mL (0.87 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (0.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Lu B, et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma. ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.